BAY-899是一种口服有效和选择性的促黄体生成激素受体(LH-R)拮抗剂，对hLH(人LH)和rLH(大鼠LH)的IC50分别为185nM和46nM。BAY-899可以降低性激素水平。
货号:ajcx32374
CAS:2471967-92-5
分子式:C25H19F2N5O2
分子量：459.45
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

BAY-899 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 185 nM and 46nM for hLH (human LH) and rLH (rat LH), respectively. BAY-899 can reduce sex hormone levels[1].

BAY-899 (oral; 12.5 mg/kg/day; for 8 days) shows an efficiency to reduce serum estradiol levels in intact female rats[1]. BAY-899 (iv of 0.5 mg/kg or po of 2 mg/kg) has a t1/2 of 11 hours and 12 hours for iv and po. And the Cmax is 0.97 kg/L and 0.24 kg/L for iv and po[1]. Animal Model: Intact female rats[1]

[1]. Wortmann L, et al. Discovery of BAY-298 and BAY-899: Tetrahydro-1,6-naphthyridine-Based, Potent and Selective Antagonists of the Luteinizing Hormone Receptor Which Reduce Sex Hormone Levels In Vivo. J Med Chem. 2019 Oct 31.